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AbstractAbstract
[en] Lanreotide (D-β-Nal-Cys-Try-D-Trp-Lys-Val-Cys-Thr-NH2) is a new somatostatin analogue. It can bind to human somatostatin receptor (hSSTR) subtype 2 through 5 with high affinity and to hSSTR subtype 1 with low affinity. We investigate labeling condition, quality control and stability in vitro of 125I-Lanreotide and 188Re-lanreotide respectively. (A) Lanreotide is labeled with 125I using Chloramine T. The effect of reaction condition (such as reaction time, pH value, Lanreotide amount, quantity of Chloramine T and reaction volume) on labeling yield is investigated in detail. (B) The labeling yield and radiochemical purity (RP) is measured with paper chromatography (PC) and Sep-Pak C18 Cartridge. For PC method, 125I-Lanreotide is spotted on the Whatman No.1 paper and developed in the mixture of CH3CH2CH2CH2OH and CH3CH2OH and NH4OH (v/v/v=5:2:1), the Rf value of every component in the mobile phase is given in table 1. For Sep-Pak C18 Cartridge methods each cartridge is washed with 10 ml of ethanol followed by 10 ml of iso-CH3CH2CH2OH solution. Aliquots of 0.1 mI sample is loaded onto the cartridge, unbound peptide (sodium iodine-125) is eluted with 5 ml of 0.5mol/L sodium acetate solution, 125I-Lanreotide is eluted with 5 mI of 95% aqueous ethanol solution. (C) The stability of 125I-Lanreotide in vitro is investigated by labeling compound incubating for 48 hours at 37 deg. C in the 0.9% sodium chloride solution and RP is tested by PC at specific time intervals. (D) Lanreotide is labeled directly with 188Re via the mixture of citrate and tartate using stannous chloride as reduced agent. The influence of reaction conditions such as pH, temperature, amount of stannous chloride, amount of Lanreotide and reaction time on labeling yield is investigated in detail. At the time, the stability in vitro quality control and animal test are evaluated
Primary Subject
Secondary Subject
Source
International Atomic Energy Agency, Vienna (Austria); 99 p; 2000; p. 31-33; Research co-ordination meeting on labelling techniques of biomolecules for targeted radiotherapy; Mumbai (India); 31 Jan - 4 Feb 2000; 3 tabs
Record Type
Report
Literature Type
Conference
Report Number
Country of publication
BETA DECAY RADIOISOTOPES, BETA-MINUS DECAY RADIOISOTOPES, DAYS LIVING RADIOISOTOPES, DRUGS, ELECTRON CAPTURE RADIOISOTOPES, HEAVY NUCLEI, HOURS LIVING RADIOISOTOPES, INTERMEDIATE MASS NUCLEI, INTERNAL CONVERSION RADIOISOTOPES, IODINE ISOTOPES, ISOMERIC TRANSITION ISOTOPES, ISOTOPES, KINETICS, LABELLED COMPOUNDS, MATERIALS, MEDICINE, MINUTES LIVING RADIOISOTOPES, NUCLEAR MEDICINE, NUCLEI, ODD-EVEN NUCLEI, ODD-ODD NUCLEI, ORGANIC COMPOUNDS, PROTEINS, RADIOACTIVE MATERIALS, RADIOISOTOPES, RADIOLOGY, RHENIUM ISOTOPES, SEPARATION PROCESSES, THERAPY, YIELDS
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